Inclusion complex of cyclodextrin and indomethacin and a process

Details Inclusion complex of cyclodextrin and indomethacin and a process Inclusion complex of cyclodextrin and indomethacin and a process

1979-01-24

1980-10-14

Friedman, Stanley J.

Drug, bio-affecting and body treating compositions

Conjugate or complex of monoclonal or polyclonal antibody,...

Conjugated via claimed linking group, bond, chelating agent,...

536103, A61K 3170, C08B 3716

Patent

active

042281601

ABSTRACT:
The invention relates to an inclusion complex of 1-(p-chloro-benzoyl)-5-methoxy-2-methyl-indol-3-yl-acetic acid (indomethacin) and cyclodextrin of a molar ratio of about 2:1. The inclusion complex can be prepared by reacting about 2 moles of alpha or beta cyclodextrin with about 1 mole of 1-(p-chloro-benzoyl)-5-methoxy-2-methyl-indol-3-yl-acetic acid under heating in the presence of an organic solvent which dissolves indomethacin and does not form a stable complex with cyclodextrin. The new complex is at least as active antiinflammatory agent as indomethacin and at the same time shows substantially less ulcerative side-effect.

REFERENCES:
patent: 2959580 (1960-11-01), Schlenk et al.
patent: 3061444 (1962-10-01), Rogers et al.
patent: 4054736 (1977-10-01), Hayashi et al.
Frank, Sylvan G., Journal of Pharmaceutical Sciences, Oct. 1975, p. 1585.
Agr. Biol. Chem., vol. 34, No. 12, pp. 1787-1794 (1970).
Hamada et al., Chem. Pharm. Bull., 23, 1205 (1975).
Kurozumi et al., Chem. Pharm. Bull., 23, 3062 (1975).

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